Glycyrrhetinic Acid Ammonium Loaded Microspheres Using Colocasia esculenta and Bombax ceiba mucilages: In Vitro and In Vivo Characterization

Background: Glycyrrhetinic acid ammonium (GAA) inhibits the biosynthesis of prostaglandins PGE-2 and PGF-2α to their inactive metabolites. This causes an increased level of prostaglandins in the digestive system which inhibit gastric secretion. Objective: The aim of the present investigation was to develop mucoadhesive microspheres of GAA using Colocasia esculenta (CE) and Bombax ceiba (BC) mucilages, alone and in combination for the efficient treatment of gastric ulcer. Methods: The glycyrrhetinic acid (GA) was extracted as ammonium salt from dried stolons of Glycyrrhiza glabra using hot maceration technique. Extraction of mucilage was carried out using herbs and rhizomes of CE and flowers of BC by cold maceration method. The hydrophilic molecule of GAA was encapsulated using single phase emulsification technique. Glutaraldehyde was used as cross-linking agent. The developed microspheres were evaluated for morphology, particle size, entrapment efficiency, drug loading, in vitro mucoadhesion, swelling behavior, in vitro drug release and in vivo ulcer healing activity. Results: The results showed that the drug-polymer in 1: 2 ratio in CE- mucilage containing microspheres exhibited prolonged drug release as compared to BC-mucialge or their combination. The stability study results showed stable character of GAA in the developed microspheres. The developed microspheres show effective in vivo ulcer healing activity in Wistar male albino rats. Conclusion: The preliminary results of this study suggest that the developed mucoadhesive microspheres containing GAA could be a promising tool in the treatment of gastric ulcer and can be advantageous over the conventional anti ulcer therapy. The study also suggested that the extracted mucilages can be used in the preparation of the mucoadhesive microspheres.